| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
GnRH
Goserelin targets GnRH receptors (GnRHR) in the pituitary gland. It binds to GnRHR with a Kᵢ of 1.6 nM in CHO cells expressing the human receptor. Short-term administration stimulates gonadotropin and sex hormone release, while continuous administration causes suppression of gonadotropin secretion. |
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| ln Vitro |
Goserelin (1 nM-1 mM; 48-72 hours) promotes expression in EOC cells [1]. Goserelin (100 μM; 24-72 hours) regulates the expression of human liver cancer-related genes in SKOV3-ip cells [1]. (100 μM; 24-72 hours) promotes EOC cell inflammation by upregulating FOXO1 through PI3K/AKT signaling [1]. Apoptosis analysis [1] Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell line) Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM Incubation time : 48 hours, 72 hours results: significantly increased the total apoptosis rate of SKOV3-ip, SKOV3 and A2780 cells. Western Blot Analysis[1] Cell lines: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell line) Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM Incubation time: Results at 48 hours and 72 hours: At 100 μM, the expression of cleaved-caspase-3 and cleaved-PARP increased significantly. RT-PCR[1] Cell line: SKOV3-ip Cell concentration: 100 μM Incubation time: 24 hours, 48 hours, 72 hours Results: Expression of human apoptosis-related genes is regulated
In vitro, goserelin binds to GnRH receptors and activates them, stimulating gonadotropin release. It is a synthetic decapeptide analogue of LHRH with antineoplastic activity. The compound's activity is mediated through GnRH receptor binding and signaling. |
| ln Vivo |
Goserelin acetate (100 μg; subcutaneous injection; daily; for 19 days) significantly increases the proportion of anode cells in subcutaneous xenograft tumors [1]. Animal model: Five-week-old specific pathogen-free (SPF) female nude mice (18-20 g), subcutaneous xenograft tumor model [1] Dosage: 100 µg/mouse Administration: subcutaneous injection, daily, for 19 days Results : Significantly increases the proportion of apoptotic cells in subcutaneous xenograft tumors
In vivo, continuous, prolonged administration of goserelin in males results in inhibition of pituitary gonadotropin secretion, leading to a significant decline in testosterone production. In females, prolonged administration results in a decrease in estradiol production. The compound is used to treat hormone-sensitive cancers (breast, prostate, ovarian) and endometriosis. |
| Enzyme Assay |
GnRH receptor binding assays: Membranes from CHO cells expressing human GnRH receptors are incubated with radiolabeled GnRH analog and goserelin at various concentrations (typically 0.1-100 nM). Binding affinity (Kᵢ) is calculated from displacement curves. Functional assays measure gonadotropin release from pituitary cells or cell lines expressing GnRH receptors.
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| Cell Assay |
Cell Line: SKOV3 cells, SKOV3-ip cells, A2780 cells (human EOC cell lines)
Concentration: 1 nM, 10 nM, 100 nM, 1 μM, 10 μM, 100 μM, 1 mM Incubation Time: 48 hours, 72 hours Result: Significantly increased the total apoptosis rate of SKOV3-ip, SKOV3 and A2780 cells GnRH receptor-expressing cells (e.g., CHO cells or pituitary cell lines) are cultured in appropriate media at 37°C with 5% CO₂. Cells are treated with goserelin at various concentrations. Receptor activation is assessed by measuring cAMP levels or downstream signaling. Gonadotropin release is measured by ELISA or radioimmunoassay. |
| Animal Protocol |
Five-week-old specific-pathogen free (SPF) female nude mice (18-20 g), subcutaneous xenograft tumor model
100 µg/mice Subcutaneous injection, daily, for 19 days In vivo studies are conducted in animal models or clinical trials. Goserelin acetate is administered via subcutaneous or intramuscular injection at doses determined by the specific protocol. Hormone levels (testosterone, estradiol, LH, FSH) are measured in blood samples. Tumor growth is monitored in xenograft or patient studies. Efficacy in endometriosis is assessed by symptom improvement. |
| ADME/Pharmacokinetics |
Goserelin acetate has molecular formula C₅₉H₈₄N₁₈O₁₄·C₂H₄O₂ (or C₆₁H₈₈N₁₈O₁₆). It is a synthetic decapeptide analog of LHRH. The compound is administered via injection.
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| References |
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| Additional Infomation |
According to state or federal labeling requirements, goserelin acetate can cause developmental toxicity, female reproductive toxicity, and male reproductive toxicity. Goserelin acetate is the acetate of a synthetic decapeptide analog of luteinizing hormone-releasing hormone (LHRH). Long-term continuous use of goserelin in men can suppress pituitary gonadotropin secretion, leading to a significant decrease in testosterone production; long-term use in women can lead to a decrease in estradiol production. (NCI04) Goserelin is a synthetic, long-acting gonadotropin-releasing hormone agonist. It is used to treat prostate cancer, uterine fibroids, and metastatic breast cancer. See also: Goserelin (containing the active portion).
Goserelin acetate is a synthetic GnRH agonist used to treat hormone-sensitive cancers and endometriosis. Continuous administration suppresses gonadotropin secretion, leading to decreased sex hormone production. It is available as an injectable formulation under the brand name Zoladex. The compound has been approved for clinical use in breast cancer, prostate cancer, epithelial ovarian cancer, and endometriosis. |
| Molecular Formula |
C61H88N18O16
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|---|---|
| Molecular Weight |
1329.485
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| Exact Mass |
1328.66
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| Elemental Analysis |
C, 55.11; H, 6.67; N, 18.96; O, 19.25
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| CAS # |
145781-92-6
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| Related CAS # |
Goserelin; 65807-02-5
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| PubChem CID |
16052011
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
1695.5ºC at 760mmHg
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| Melting Point |
>190°C (dec.)
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.692
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| LogP |
-0.95
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| Hydrogen Bond Donor Count |
18
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
32
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| Heavy Atom Count |
95
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| Complexity |
2590
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| Defined Atom Stereocenter Count |
9
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| SMILES |
O=C(N[C@H](C(N[C@@H](CC1=CC=C(O)C=C1)C(N[C@H](COC(C)(C)C)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N2CCC[C@H]2C(NNC(N)=O)=O)=O)=O)=O)=O)=O)CO)[C@@H](NC([C@H](CC3=CN=CN3)NC([C@@H](N4)CCC4=O)=O)=O)CC5=CNC6=C5C=CC=C6.CC(O)=O
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| InChi Key |
IKDXDQDKCZPQSZ-JHYYTBFNSA-N
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| InChi Code |
InChI=1S/C59H84N18O14.C2H4O2/c1-31(2)22-40(49(82)68-39(12-8-20-64-57(60)61)56(89)77-21-9-13-46(77)55(88)75-76-58(62)90)69-54(87)45(29-91-59(3,4)5)74-50(83)41(23-32-14-16-35(79)17-15-32)70-53(86)44(28-78)73-51(84)42(24-33-26-65-37-11-7-6-10-36(33)37)71-52(85)43(25-34-27-63-30-66-34)72-48(81)38-18-19-47(80)67-38;1-2(3)4/h6-7,10-11,14-17,26-27,30-31,38-46,65,78-79H,8-9,12-13,18-25,28-29H2,1-5H3,(H,63,66)(H,67,80)(H,68,82)(H,69,87)(H,70,86)(H,71,85)(H,72,81)(H,73,84)(H,74,83)(H,75,88)(H4,60,61,64)(H3,62,76,90);1H3,(H,3,4)/t38-,39-,40-,41-,42-,43-,44-,45+,46-;/m0./s1
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| Chemical Name |
acetic acid;(2S)-N-[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2R)-1-[[(2S)-1-[[(2S)-1-[(2S)-2-[(carbamoylamino)carbamoyl]pyrrolidin-1-yl]-5-(diaminomethylideneamino)-1-oxopentan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-3-[(2-methylpropan-2-yl)oxy]-1-oxopropan-2-yl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-3-hydroxy-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]-5-oxopyrrolidine-2-carboxamide
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| Synonyms |
Goserelin Acetate; ICI-118630; ICI118630; ICI 118630; brand name: Zoladex
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
H2O: ~100 mg/mL (~75.2 mM)
DMSO: ≥ 28 mg/mL (~21.1 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (1.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (1.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 2.08 mg/mL (1.56 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (37.61 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.7522 mL | 3.7608 mL | 7.5217 mL | |
| 5 mM | 0.1504 mL | 0.7522 mL | 1.5043 mL | |
| 10 mM | 0.0752 mL | 0.3761 mL | 0.7522 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Treating Prostate Cancer That Has Come Back After Surgery With Apalutamide and Targeted Radiation Based on PET Imaging
CTID: NCT04423211
Phase: Phase 3 Status: Recruiting
Date: 2024-11-05
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Products are for research use only; We do not sell to patients
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